NCIt definition : An orally bioavailable, small molecule inhibitor of signaling transducer and activator
3 (STAT3), with potential antineoplastic and immunomodulatory activities. Upon administration,
STAT3 inhibitor WP1066 blocks the intranuclear translocation of p-STAT, thereby suppressing
STAT3 signaling and decreasing the levels of downstream products including c-Myc.
Additionally, WP1066 may upregulate costimulatory molecules including CD80 and CD86
on human microglia, and reverse glioma cancer stem cell (gCSC)-mediated innate and
adaptive immune suppression allowing for the restoration of antitumor effector immune
responses. The STAT3 pathway is overly active in many cancer types and is implicated
in CSC-mediated growth, recurrence and resistance to conventional chemotherapies.;